Balanced AT1/AT2 receptor antagonists. 4. XR510 and related 5-(3- amidopropanoyl)imidazoles possessing equal affinity for the AT1 and AT2 receptors

Article abstract of DOI:10.1021/jm00015a016

The identification of the AT₁ and AT₂ receptor subtypes has stimulated interest in developing balanced angiotensin II receptor antagonists. A series of 5-(3-amidopropanoyl)imidazoles has been prepared which possess balanced affinity for the AT₁ and AT₂ receptors. XR510 (1), 1-[[2'- [[(isopentoxycarbonyl)amino]sulfonyl]-3-fluoro(1,1'-biphenyl)-4-yl]methyl]- 5-[3-(N-pyridin-3-ylbutanamido)propanoyl]-4-ethyl-2-propyl-1H-imidazole, potassium salt, exhibits subnanomolar affinity for both receptor sites. XR510 is very active in lowering blood pressure in renal hypertensive rats and furosemide-treated dogs following oral administration.